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  • 學位論文

設計與合成比咯苯偶氮駢A環結合 Enediyne之混成試劑

Design and Synthesis of Hybrid Agents Based upon Pyrrolo[2,1-c][1,4]benzodiazepine A-ring Linked with Enediyne

指導教授 : 王志鉦
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摘要


比咯苯偶氮駢(pyrrolo[2,1-c][1,4]benzodiazpines , PBDs)是鏈球菌屬所分離出來的一種很強的抗癌烷化試劑和基因導向試劑。另一種藥物烯雙炔(enediyne)主要是鏈球菌之代謝物所分離出來的,其生物活性主要來自於雙電子中間體所產生的特定形式。 在本論文中,我們報告設計與合成PBD-enediyne混成試劑,這類混成試劑的合成主要是運用DC-81來聯接多樣性之enediyne。在這8個PBD-enediyne結合中,所獲得產率在2.6% 至9.8%。

關鍵字

咯苯偶氮駢

並列摘要


pyrrolo[2,1-c][1,4]benzodiazpines (PBDs) are a group of potent naturally occurring antitumor alkylating agents produced by Streptomyces species.Enediyne was either isolated or derived from Streptomyces, which are sourced from a specific generation mode of diradical intermediates. In this thesis, we report the design and synthesis of PBD-enediyne conjugate agents. The synthesis of these conjugates was carried out of DC-81 coupled with a variety of enediyne. There were 8 PBD-enediyne conjugates obtained in 2.6% ~ 9.8% yields.

並列關鍵字

PBDs

參考文獻


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